KR100754236B1 - 라파마이신 유도체의 지향선택적 합성방법 - Google Patents

라파마이신 유도체의 지향선택적 합성방법 Download PDF

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Publication number
KR100754236B1
KR100754236B1 KR1020027004033A KR20027004033A KR100754236B1 KR 100754236 B1 KR100754236 B1 KR 100754236B1 KR 1020027004033 A KR1020027004033 A KR 1020027004033A KR 20027004033 A KR20027004033 A KR 20027004033A KR 100754236 B1 KR100754236 B1 KR 100754236B1
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South Korea
Prior art keywords
rapamycin
acid
carbon atoms
ether
ester
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Expired - Fee Related
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KR1020027004033A
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English (en)
Korean (ko)
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KR20020029796A (ko
Inventor
쇼츠아-청
셀스테트존해밀튼
누렐뎅라자크
칠글로리아카렌
포르티에쥬느비에브
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와이어쓰
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020027004033A 1999-09-29 2000-09-27 라파마이신 유도체의 지향선택적 합성방법 Expired - Fee Related KR100754236B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US40883099A 1999-09-29 1999-09-29
US09/408,830 1999-09-29

Publications (2)

Publication Number Publication Date
KR20020029796A KR20020029796A (ko) 2002-04-19
KR100754236B1 true KR100754236B1 (ko) 2007-09-03

Family

ID=23617953

Family Applications (1)

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KR1020027004033A Expired - Fee Related KR100754236B1 (ko) 1999-09-29 2000-09-27 라파마이신 유도체의 지향선택적 합성방법

Country Status (24)

Country Link
EP (1) EP1216251B1 (cg-RX-API-DMAC7.html)
JP (1) JP4289813B2 (cg-RX-API-DMAC7.html)
KR (1) KR100754236B1 (cg-RX-API-DMAC7.html)
CN (1) CN1176925C (cg-RX-API-DMAC7.html)
AR (1) AR029181A1 (cg-RX-API-DMAC7.html)
AT (1) ATE233269T1 (cg-RX-API-DMAC7.html)
AU (1) AU782234B2 (cg-RX-API-DMAC7.html)
BR (1) BR0014433A (cg-RX-API-DMAC7.html)
CA (1) CA2385461C (cg-RX-API-DMAC7.html)
CZ (1) CZ300368B6 (cg-RX-API-DMAC7.html)
DE (1) DE60001510T2 (cg-RX-API-DMAC7.html)
DK (1) DK1216251T3 (cg-RX-API-DMAC7.html)
EA (1) EA004331B1 (cg-RX-API-DMAC7.html)
ES (1) ES2189768T3 (cg-RX-API-DMAC7.html)
HK (1) HK1044774B (cg-RX-API-DMAC7.html)
HU (1) HUP0202609A3 (cg-RX-API-DMAC7.html)
IL (2) IL148542A0 (cg-RX-API-DMAC7.html)
MX (1) MXPA02003243A (cg-RX-API-DMAC7.html)
NO (1) NO20021360L (cg-RX-API-DMAC7.html)
NZ (1) NZ517644A (cg-RX-API-DMAC7.html)
PL (1) PL200899B1 (cg-RX-API-DMAC7.html)
TW (1) TWI256395B (cg-RX-API-DMAC7.html)
WO (1) WO2001023395A2 (cg-RX-API-DMAC7.html)
ZA (1) ZA200201918B (cg-RX-API-DMAC7.html)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070032853A1 (en) 2002-03-27 2007-02-08 Hossainy Syed F 40-O-(2-hydroxy)ethyl-rapamycin coated stent
US20050118344A1 (en) 2003-12-01 2005-06-02 Pacetti Stephen D. Temperature controlled crimping
AU2004270154A1 (en) * 2003-09-03 2005-03-17 Wyeth Amorphous rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid and its pharmaceutical compositions containing the same
AR046194A1 (es) 2003-11-04 2005-11-30 Mayo Foundation Metodo de tratamiento del linfoma de celulas del manto
EP1751168A1 (en) 2004-04-14 2007-02-14 Wyeth Proline cci-779 (proline-rapamycin 42-ester with 2,2-bis (hydroxymethyl) propionic acid) and two-step enzymatic synthesis of proline cci-779 and cci-779 using microbial lipase
CN1942476A (zh) * 2004-04-14 2007-04-04 惠氏公司 纳巴霉素42－酯衍生物的区位特异合成
MX2007001676A (es) 2004-08-10 2007-04-12 Wyeth Corp Derivados de 42-ester de rapamicina con acido 2,2-bis(hidroximetil)propionico y metodos para hacer los mismos.
DE602006021142D1 (de) 2005-02-03 2011-05-19 Gen Hospital Corp Verfahren zur behandlung von gefitinib-resistentem krebs
WO2006086172A1 (en) 2005-02-09 2006-08-17 Wyeth Cci-779 polymorph and use thereof
PE20070763A1 (es) 2005-11-04 2007-08-08 Wyeth Corp COMBINACIONES ANTINEOPLASICAS DE UN INHIBIDOR DE mTOR, TRASTUZUMAB Y/O HKI-272
US8022216B2 (en) 2007-10-17 2011-09-20 Wyeth Llc Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof
ES2692769T3 (es) 2008-06-17 2018-12-05 Wyeth Llc Combinaciones antineoplásicas que contienen HKI-272 y vinorelbina
CN101676291B (zh) 2008-09-18 2012-05-09 上海海和药物研究开发有限公司 一类雷帕霉素碳酸酯类似物、其药物组合物及其制备方法和用途
WO2011092564A2 (en) * 2010-01-28 2011-08-04 Fresenius Kabi Oncology Ltd Process for the preparation of temsirolimus and its intermediates
CN102020662B (zh) 2011-01-07 2013-02-13 天津市炜杰科技有限公司 一种驮瑞塞尔制备方法
BR112013025085A2 (pt) * 2011-04-01 2016-07-19 Sandoz Ag processo para a acilação de rapamicina e processo para sintetizar tensirolimo
CN103421023B (zh) * 2013-07-30 2015-09-23 福建省微生物研究所 一种替西罗莫司的合成工艺
CN104086564B (zh) * 2014-07-30 2019-02-05 江苏奥赛康药业股份有限公司 一种高纯度坦罗莫司的制备方法
CN106146536B (zh) * 2015-04-25 2019-07-26 山东新时代药业有限公司 一种依维莫司的制备方法
CA3017690C (en) * 2016-03-14 2024-02-20 Wisconsin Alumni Research Foundation Oligolactic acid conjugates and micelles with enhanced anticancer efficacy
CN107561170B (zh) * 2016-07-02 2021-07-30 山东新时代药业有限公司 一种坦西莫司中间体的分析检测方法
CN108948046B (zh) * 2017-05-20 2020-11-10 鲁南制药集团股份有限公司 一种替西罗莫司的中间体及其制备方法
CN108948045A (zh) * 2017-05-20 2018-12-07 鲁南制药集团股份有限公司 一种替西罗莫司的制备方法
CN109206441B (zh) * 2017-06-30 2022-05-20 正大天晴药业集团股份有限公司 一种依维莫司的纯化方法
CN109776570A (zh) * 2017-11-14 2019-05-21 上海医药工业研究院 一种依维莫司中间体、其制备方法及其应用
EA202092692A1 (ru) 2018-06-15 2021-04-21 Навитор Фармасьютикалз, Инк. Аналоги рапамицина и их применения
CN109369679A (zh) * 2018-12-24 2019-02-22 江苏卓和药业有限公司 一种雷帕霉素的精制方法
CN109851626B (zh) * 2019-01-08 2021-11-02 扬子江药业集团四川海蓉药业有限公司 一种替西罗莫司的分离纯化方法
CN115209897A (zh) 2019-12-05 2022-10-18 安纳库利亚治疗公司 雷帕霉素类似物及其用途
CN113372359A (zh) * 2020-03-10 2021-09-10 鲁南制药集团股份有限公司 一种坦西莫司的制备方法
CN114106014B (zh) * 2020-08-27 2024-03-15 鲁南制药集团股份有限公司 一种依维莫司的制备方法
CN115028658A (zh) * 2022-07-06 2022-09-09 国药集团川抗制药有限公司 雷帕霉素硅醇酯及其制备方法和应用

Citations (3)

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Publication number Priority date Publication date Assignee Title
US5362718A (en) * 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
US5387680A (en) * 1993-08-10 1995-02-07 American Home Products Corporation C-22 ring stabilized rapamycin derivatives
US5563145A (en) * 1994-12-07 1996-10-08 American Home Products Corporation Rapamycin 42-oximes and hydroxylamines

Family Cites Families (1)

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Publication number Priority date Publication date Assignee Title
US5120842A (en) * 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5387680A (en) * 1993-08-10 1995-02-07 American Home Products Corporation C-22 ring stabilized rapamycin derivatives
US5362718A (en) * 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
US5563145A (en) * 1994-12-07 1996-10-08 American Home Products Corporation Rapamycin 42-oximes and hydroxylamines

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AR029181A1 (es) 2003-06-18
DE60001510D1 (de) 2003-04-03
HUP0202609A3 (en) 2004-11-29
JP2003510329A (ja) 2003-03-18
CN1402731A (zh) 2003-03-12
HK1044774B (en) 2003-05-30
PL354461A1 (en) 2004-01-12
AU7718200A (en) 2001-04-30
ATE233269T1 (de) 2003-03-15
CN1176925C (zh) 2004-11-24
DK1216251T3 (da) 2003-06-16
CZ300368B6 (cs) 2009-05-06
ES2189768T3 (es) 2003-07-16
JP4289813B2 (ja) 2009-07-01
NZ517644A (en) 2003-09-26
MXPA02003243A (es) 2002-09-30
CZ20021136A3 (cs) 2002-06-12
NO20021360D0 (no) 2002-03-19
IL148542A0 (en) 2002-09-12
AU782234B2 (en) 2005-07-14
CA2385461C (en) 2009-03-17
PL200899B1 (pl) 2009-02-27
WO2001023395A3 (en) 2001-10-25
ZA200201918B (en) 2003-08-27
EP1216251B1 (en) 2003-02-26
KR20020029796A (ko) 2002-04-19
NO20021360L (no) 2002-03-19
IL148542A (en) 2006-08-20
EA004331B1 (ru) 2004-04-29
CA2385461A1 (en) 2001-04-05
BR0014433A (pt) 2002-06-11
WO2001023395A2 (en) 2001-04-05
HUP0202609A2 (hu) 2002-12-28
EA200200412A1 (ru) 2002-10-31
EP1216251A2 (en) 2002-06-26
DE60001510T2 (de) 2003-10-02
HK1044774A1 (en) 2002-11-01
TWI256395B (en) 2006-06-11

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